Osmaniye Derya, Sağlık Begüm Nurpelin, Khalilova Narmin, Levent Serkan, Bayazıt Gizem, Gül Ülküye Dudu, Özkay Yusuf, Kaplancıklı Zafer Asım
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, 26470 Eskişehir, Turkey.
Doping and Narcotic Compounds Analysis Laboratory, Faculty of Pharmacy, Anadolu University, 26470 Eskişehir, Turkey.
ACS Omega. 2023 Feb 13;8(7):6669-6678. doi: 10.1021/acsomega.2c07256. eCollection 2023 Feb 21.
Cancer is a progressive disease that is frequently encountered worldwide. The incidence of cancer is increasing with the changing living conditions around the world. The side-effect profile of existing drugs and the resistance developing in long-term use increase the need for novel drugs. In addition, cancer patients are not resistant to bacterial and fungal infections due to the suppression of the immune system during the treatment. Rather than adding a new antibacterial or antifungal drug to the current treatment plan, the fact that the drug with anticancer activity has these effects (antibacterial and antifungal) will increase the patient's quality of life. For this purpose, in this study, a series of 10 new naphthalene-chalcone derivatives were synthesized and their anticancer-antibacterial-antifungal properties were investigated. Among the compounds, compound showed activity against the A549 cell line with an IC = 7.835 ± 0.598 μM. This compound also has antibacterial and antifungal activity. The apoptotic potential of the compound was measured by flow cytometry and showed apoptotic activity of 14.230%. The compound also showed 58.870% mitochondrial membrane potential. Compound inhibited VEGFR-2 enzyme with IC = 0.098 ± 0.005 μM. Molecular docking studies of the compounds were carried out by methods against VEGFR-2 and caspase-3 enzymes.
癌症是一种在全球范围内经常遇到的进行性疾病。随着世界各地生活条件的变化,癌症的发病率正在上升。现有药物的副作用以及长期使用中产生的耐药性增加了对新型药物的需求。此外,癌症患者在治疗期间由于免疫系统受到抑制,对细菌和真菌感染没有抵抗力。如果具有抗癌活性的药物具有这些(抗菌和抗真菌)作用,而不是在当前治疗方案中添加新的抗菌或抗真菌药物,将提高患者的生活质量。为此,在本研究中,合成了一系列10种新的萘-查尔酮衍生物,并研究了它们的抗癌-抗菌-抗真菌特性。在这些化合物中,化合物 对A549细胞系表现出活性,IC = 7.835 ± 0.598 μM。该化合物还具有抗菌和抗真菌活性。通过流式细胞术测量该化合物的凋亡潜力,显示凋亡活性为14.230%。该化合物还显示出线粒体膜电位为58.870%。化合物 以IC = 0.098 ± 0.005 μM抑制VEGFR-2酶。通过 方法对化合物进行了针对VEGFR-2和caspase-3酶的分子对接研究。